Lipoprotein-mimicking solid lipid nanoparticles for drug delivery and uses thereof
AssigneeTionlab Therapeutics
InventorsDuck Soo Lim, Jin-Ho Kim
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Abstract
According to the present invention, it is possible to provide a drug carrier having excellent bioavailability and improved drug encapsulation efficiency by preparing lipoprotein-mimicking solid lipid nanoparticles having a core-shell structure consisting of albumin-conjugated cholesterol, a fusogenic lipid, a cationic lipid, a triglyceride and a cholesteryl ester.
Claims20
A high-density lipoprotein (HDL)-mimicking solid lipid nanoparticle comprising:
- a core comprising a triglyceride and a cholesteryl ester;
- and
- a shell comprising albumin-conjugated cholesterol, a fusogenic lipid and a cationic lipid;
- wherein the albumin-conjugated cholesterol is a reaction product of cholesteryl chloroformate and albumin;
- wherein the shell is substantially free of apolipoproteins;
- wherein the HDL-mimicking solid lipid nanoparticle comprises, based on 100 parts by weight in total:
- 10 to 25 parts by weight of the cholesteryl ester,
- 0.01 to 5 parts by weight of the triglyceride,
- 1 to 20 parts by weight of the albumin-conjugated cholesterol,
- 5 to 40 parts by weight of the fusogenic lipid, and
- 10 to 60 parts by weight of the cationic lipid.
A method for preparing high-density lipoprotein (HDL)-mimicking solid lipid nanoparticles, the method comprising preparing an aqueous dispersion in which HDL-mimicking solid lipid nanoparticles are dispersed by mixing a cholesteryl ester, a triglyceride, albumin-conjugated cholesterol, a fusogenic lipid and a cationic lipid in an organic solvent;
- wherein the shell is substantially free of apolipoproteins;
- wherein the HDL-mimicking solid lipid nanoparticle comprises, based on 100 parts by weight in total:
- 10 to 25 parts by weight of the cholesteryl ester,
- 0.01 to 5 parts by weight of the triglyceride,
- 1 to 20 parts by weight of the albumin-conjugated cholesterol,
- 5 to 40 parts by weight of the fusogenic lipid, and
- 10 to 60 parts by weight of the cationic lipid.
Dependencies are inferred from the claim text.